title: Interaction of the efflux transporters ABCB1 and ABCG2 with imatinib, nilotinib, and dasatinib.
abstract: The efflux transporters adenosine triphosphate (ATP)-binding cassette (ABC)B1 and ABCG2 have been demonstrated to interact with the tyrosine kinase inhibitors (TKIs) imatinib, nilotinib, and dasatinib. However, although some studies conclude that TKIs are substrates of one or both transporters, other studies demonstrate only an inhibitory function. This variation is probably due to differences in the concentration of TKIs assayed and the experimental systems used. This article examines the evidence for clinically relevant interactions between three currently approved TKIs and ABCB1/ABCG2.
authors.affiliation: 1] Cancer Theme, South Australian Health and Medical Research Institute, Adelaide, South Australia, Australia [2] Department of Medicine, University of Adelaide, Adelaide, South Australia, Australia.
authors.forename: L N
authors.initials: LN
authors.lastname: Eadie
authors.affiliation: 1] Cancer Theme, South Australian Health and Medical Research Institute, Adelaide, South Australia, Australia [2] Department of Medicine, University of Adelaide, Adelaide, South Australia, Australia [3] Centre for Cancer Biology, Adelaide, South Australia, Australia.
authors.forename: T P
authors.initials: TP
authors.lastname: Hughes
authors.affiliation: 1] Cancer Theme, South Australian Health and Medical Research Institute, Adelaide, South Australia, Australia [2] Department of Medicine, University of Adelaide, Adelaide, South Australia, Australia [3] Centre for Cancer Biology, Adelaide, South Australia, Australia.
authors.forename: D L
authors.initials: DL
authors.lastname: White
mesh_terms: D018435:ATP Binding Cassette Transporter, Subfamily B; D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1 / Q000378:metabolism*; D000070997:ATP Binding Cassette Transporter, Subfamily G, Member 2; D018528:ATP-Binding Cassette Transporters / Q000378:metabolism*; D000818:Animals; D001549:Benzamides / Q000378:metabolism*; D000069439:Dasatinib; D004791:Enzyme Inhibitors / Q000378:metabolism*; D006801:Humans; D000068877:Imatinib Mesylate; D009363:Neoplasm Proteins / Q000378:metabolism*; D010879:Piperazines / Q000378:metabolism*; D011505:Protein-Tyrosine Kinases / Q000037:antagonists & inhibitors*; D011743:Pyrimidines / Q000378:metabolism*; D013844:Thiazoles / Q000378:metabolism*
chemical_list: C513055:ABCB1 protein, human; C116614:ABCG2 protein, human; D018435:ATP Binding Cassette Transporter, Subfamily B; D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1; D000070997:ATP Binding Cassette Transporter, Subfamily G, Member 2; D018528:ATP-Binding Cassette Transporters; D001549:Benzamides; D004791:Enzyme Inhibitors; D009363:Neoplasm Proteins; D010879:Piperazines; D011743:Pyrimidines; D013844:Thiazoles; D000068877:Imatinib Mesylate; D011505:Protein-Tyrosine Kinases; C498826:nilotinib; D000069439:Dasatinib